Bioactivity | GZR18 is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC50 of 0.677 nM. GZR18 ameliorates type 2 diabetes[1]. |
Target | EC50: 0.677 nM (GLP-1 Receptor) |
Invitro | GZR18 (30-90 nM,0.5-1 h) 剂量依赖性地刺激小鼠胰岛 β 细胞的葡萄糖依赖性胰岛素分泌[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> GZR18 相关抗体: |
In Vivo | GZR18 (0-100 nmol/kg,皮下注射,单剂量或 11 次注射) 在 db/db 小鼠糖尿病模型中降低小鼠的血糖水平,减轻小鼠体重,具有控制血糖的作用[1]。GZR18 (60 μg/kg,静脉注射或皮下注射,单剂量) 在食蟹猴模型中展现出良好的药代动力学特性[1]。GZR18 在食蟹猴模型中的药代动力学特征[1]route |
Sequence | His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys(Ala-Glu-Glu-Ala-Ala-Glu-Glu-Ala-gammaGlu-C22 diacid)-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly |
Shortening | HGEGTFTSDVSSYLEGQAA-K(AEEA-AEEA-gammaGlu-C22 diacid)-EFIAWLVRGRG |
Formula | C189H295N45O59 |
Molar Mass | 4141.63 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Zhang M, et al., GZR18, a novel long-acting GLP-1 analog, demonstrated positive in vitro and in vivo pharmacokinetic and pharmacodynamic characteristics in animal models. Eur J Pharmacol. 2022 Aug 5;928:175107. |